Netarsudil (AR-13324) 2HCl

Catalog No.S8226

Netarsudil (AR-13324) 2HCl Chemical Structure

Molecular Weight(MW): 526.45

Netarsudil (a.k.a. AR-13324) is ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.

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Biological Activity

Description Netarsudil (a.k.a. AR-13324) is ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.
Targets
norepinephrine transporter (NET) [3] ROCK [1]
2 nM(Ki)
Assay
Methods Test Index PMID
Western blot
ATM / p-ATM / ATR / p-ATR / CHK1 / p-CHK1 / p-CHK2 / BRCA1 / FANCD2 / γ-H2AX ; 

PubMed: 23405159     


The steady-state levels of the kinase ATR and its phosphorylated form are increased in Melphalan resistant cells. Conversely, ATM is constitutively downregulated in the same cells. Rather than activation of CHK1, increased steady-state phosphorylation of pCHK2 was observed in resistant cells. Notably, high dose Melphalan strongly activates CHK2 in both sensitive and resistant cells but was consistently higher in resistant cells. Moreover, BRCA1, which is slightly induced in resistant cells, becomes markedly reduced in both sensitive and resistant cells after high dose Melphalan indicating temporary downregulation of HRR. Also note the the lack of apparent monoubiquitinylation of FANCD2 (B). b-actin was used as reference for quantitative analysis.

23405159
Growth inhibition assay
Cell viability ; 

PubMed: 30925767     


Melphalan-induced growth inhibition of 7 HMCLs. Seven HMCLs were treated with serial concentrations of melphalan and the percentage of viable cells compared to untreated control remaining 4 days after the onset of treatment was assessed by the ATP cell titer glo assay. Results are mean values ± standard deviation (SD) of 3 separate experiments. The inhibitory concentrations leading to a 50% (IC50) or 90% (IC90) decrease in viable cells compared to untreated cells at day 4 are indicated for each cell line in the table below the figure. 

30925767
In vivo

Netarsudil primarily targets cells in the conventional outflow tract, efficiently decreasing IOP in both human and non-human primate eyes. In addition, netarsudil has been shown to increase outflow facility in non-human primate eyes and to decrease episcleral venous pressure in rabbit eyes[2].

Protocol

Solubility (25°C)

In vitro Water 54 mg/mL (102.57 mM)
DMSO 20 mg/mL (37.99 mM)
Ethanol 2 mg/mL (3.79 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 526.45
Formula

C28H27N3O3.2HCl

CAS No. 1253952-02-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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ROCK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID